Traditional chemo and radiotherapy for the treatment of tumors is limited in utility by the absence of target specificity. Methodologies employing targeted radiotherapy wherein radioisotopes are conjugated to tumor-seeking agents have been attempted to improve biological specificity. Unfortunately, very few selective agents are available for the many tumor types and where selective agents do exist, the therapeutic advantage has been minimal. Recent methodologies for treating neoplastic diseases attempt to improve specificity by employing a class of molecules called “sensitizers” that increase the sensitivity of treated cells to, for example, chemotherapy and γ-irradiation. For example, administration of drugs such as 5-fluorouracil and wortmannin has been attempted in order to increase cellular radiation sensitivity. Owing to the non-specific nature of these and other currently available “sensitizers,” however, normal, non-neoplastic cells are subject to increased chemotherapy and radiation sensitivity thus resulting in a high level of cellular toxicity. What is urgently needed are chemotherapy and radiation sensitizers having improved specificity allowing preferential sensitivity of neoplastic as compared to normal cells. The KIAA0175 inhibitors of the present invention fulfill these and other related needs.